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Synthesis and biological evaluation of a radioiodinated spiropiperidine ligand as a potential σ1 receptor imaging agent

✍ Scribed by Rui-Qin Chen; Yan Li; Qiu-Yan Zhang; Hong-Mei Jia; Winnie Deuther-Conrad; Dirk Schepmann; Jörg Steinbach; Peter Brust; Bernhard Wünsch; Bo-Li Liu

Publisher
John Wiley and Sons
Year
2010
Tongue
French
Weight
192 KB
Volume
53
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

We report the synthesis and evaluation of 1′‐(4‐[^125^I]iodobenzyl)‐3H‐spiro[isobenzofuran‐1,4′‐piperidine] ([^125^I]Spiro‐I) as a potential SPECT tracer for imaging of σ~1~ receptors. [^125^I]Spiro‐I was prepared in 55–65% isolated radiochemical yield, with radiochemical purity of >99%, via iododestannylation of the corresponding tributyltin precursor. In receptor binding studies, Spiro‐I displayed low nanomolar affinity for σ~1~ receptors (σ~1~: K~i~=2.75±0.12 nM; σ~2~: K~i~=340 nM) and high subtype selectivity (σ~2~/σ~1~=124). Biodistribution in mice demonstrated relatively high concentration of radioactivity in organs known to contain σ~1~ receptors, including the lung, kidney, heart, spleen, and brain. Administration of haloperidol 5 min prior to injection of [^125^I]Spiro‐I significantly reduced the concentration of radioactivity in the above‐mentioned organs. These findings suggest that the binding of [^125^I]Spiro‐I to σ~1~ receptors in vivo is specific. Copyright © 2010 John Wiley & Sons, Ltd.

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